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P2X7 受体作为治疗靶点的潜力,包括炎症和肿瘤进展。

The potential of P2X7 receptors as a therapeutic target, including inflammation and tumour progression.

机构信息

Autonomic Neuroscience Centre, University College Medical School, Rowland Hill Street, London, NW3 2PF, UK.

Department of Pharmacology and Therapeutics, The University of Melbourne, Melbourne, Australia.

出版信息

Purinergic Signal. 2018 Mar;14(1):1-18. doi: 10.1007/s11302-017-9593-0. Epub 2017 Nov 21.

Abstract

Seven P2X ion channel nucleotide receptor subtypes have been cloned and characterised. P2X7 receptors (P2X7R) are unusual in that there are extra amino acids in the intracellular C terminus. Low concentrations of ATP open cation channels sometimes leading to cell proliferation, whereas high concentrations of ATP open large pores that release inflammatory cytokines and can lead to apoptotic cell death. Since many diseases involve inflammation and immune responses, and the P2X7R regulates inflammation, there has been recent interest in the pathophysiological roles of P2X7R and the potential of P2X7R antagonists to treat a variety of diseases. These include neurodegenerative diseases, psychiatric disorders, epilepsy and a number of diseases of peripheral organs, including the cardiovascular, airways, kidney, liver, bladder, skin and musculoskeletal. The potential of P2X7R drugs to treat tumour progression is discussed.

摘要

已经克隆和鉴定了七种 P2X 离子通道核苷酸受体亚型。P2X7 受体(P2X7R)的特点是细胞内 C 端有额外的氨基酸。低浓度的 ATP 打开阳离子通道,有时导致细胞增殖,而高浓度的 ATP 打开大孔,释放炎症细胞因子,并导致细胞凋亡。由于许多疾病涉及炎症和免疫反应,而 P2X7R 调节炎症,因此最近人们对 P2X7R 的病理生理作用以及 P2X7R 拮抗剂治疗各种疾病的潜力产生了兴趣。这些疾病包括神经退行性疾病、精神疾病、癫痫和许多外周器官疾病,包括心血管、气道、肾脏、肝脏、膀胱、皮肤和肌肉骨骼。还讨论了 P2X7R 药物治疗肿瘤进展的潜力。

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